Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall Interactions

The number of cases of failure in the treatment of infections associated with resistant bacteria is on the rise, due to the decreasing efficacy of current antibiotics. Notably, 7α-Acetoxy-6β-hydroxyroyleanone (AHR), a diterpene isolated from different <i>Plectranthus</i> species, showed...

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Main Authors: Filipe Pereira, Teresa Figueiredo, Rodrigo F. M. de Almeida, Catarina A. C. Antunes, Catarina Garcia, Catarina P. Reis, Lia Ascensão, Rita G. Sobral, Patricia Rijo
Format: Article
Language:English
Published: MDPI AG 2020-06-01
Series:Biomolecules
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Online Access:https://www.mdpi.com/2218-273X/10/7/983
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author Filipe Pereira
Teresa Figueiredo
Rodrigo F. M. de Almeida
Catarina A. C. Antunes
Catarina Garcia
Catarina P. Reis
Lia Ascensão
Rita G. Sobral
Patricia Rijo
author_facet Filipe Pereira
Teresa Figueiredo
Rodrigo F. M. de Almeida
Catarina A. C. Antunes
Catarina Garcia
Catarina P. Reis
Lia Ascensão
Rita G. Sobral
Patricia Rijo
author_sort Filipe Pereira
collection DOAJ
description The number of cases of failure in the treatment of infections associated with resistant bacteria is on the rise, due to the decreasing efficacy of current antibiotics. Notably, 7α-Acetoxy-6β-hydroxyroyleanone (AHR), a diterpene isolated from different <i>Plectranthus</i> species, showed antibacterial activity, namely against Methicillin-resistant <i>Staphylococcus aureus</i> (MRSA) strains. The high antibacterial activity and low cytotoxicity render this natural compound an interesting alternative against resistant bacteria. The aim of this study is to understand the mechanism of action of AHR on MRSA, using the MRSA/Vancomycin-intermediate <i>S. aureus</i> (VISA) strain CIP 106760, and to study the AHR effect on lipid bilayers and on the cell wall. Although AHR interacted with lipid bilayers, it did not have a significant effect on membrane passive permeability. Alternatively, bacteria treated with this royleanone displayed cell wall disruption, without revealing cell lysis. In conclusion, the results gathered so far point to a yet undescribed mode of action that needs further investigation.
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spelling doaj.art-7eeee9dd63e346b1b0c1a4246b096ee62023-11-20T05:29:30ZengMDPI AGBiomolecules2218-273X2020-06-0110798310.3390/biom10070983Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall InteractionsFilipe Pereira0Teresa Figueiredo1Rodrigo F. M. de Almeida2Catarina A. C. Antunes3Catarina Garcia4Catarina P. Reis5Lia Ascensão6Rita G. Sobral7Patricia Rijo8Research Center for Biosciences and Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, Campo Grande, 376, 1749-024 Lisboa, PortugalDepartamento de Ciências da Vida, UCIBIO@REQUIMTE, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2825-149 Caparica, PortugalCentro de Química Estrutural, Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, PortugalCentro de Química Estrutural, Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, PortugalResearch Center for Biosciences and Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, Campo Grande, 376, 1749-024 Lisboa, PortugalInstituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, 1649-003 Lisboa, PortugalCentro de Estudos do Ambiente e do Mar (CESAM), Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, PortugalDepartamento de Ciências da Vida, UCIBIO@REQUIMTE, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2825-149 Caparica, PortugalResearch Center for Biosciences and Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, Campo Grande, 376, 1749-024 Lisboa, PortugalThe number of cases of failure in the treatment of infections associated with resistant bacteria is on the rise, due to the decreasing efficacy of current antibiotics. Notably, 7α-Acetoxy-6β-hydroxyroyleanone (AHR), a diterpene isolated from different <i>Plectranthus</i> species, showed antibacterial activity, namely against Methicillin-resistant <i>Staphylococcus aureus</i> (MRSA) strains. The high antibacterial activity and low cytotoxicity render this natural compound an interesting alternative against resistant bacteria. The aim of this study is to understand the mechanism of action of AHR on MRSA, using the MRSA/Vancomycin-intermediate <i>S. aureus</i> (VISA) strain CIP 106760, and to study the AHR effect on lipid bilayers and on the cell wall. Although AHR interacted with lipid bilayers, it did not have a significant effect on membrane passive permeability. Alternatively, bacteria treated with this royleanone displayed cell wall disruption, without revealing cell lysis. In conclusion, the results gathered so far point to a yet undescribed mode of action that needs further investigation.https://www.mdpi.com/2218-273X/10/7/9837α-Acetoxy-6β-hydroxyroyleanoneMRSAantibacterial activitymembrane interactioncell wall
spellingShingle Filipe Pereira
Teresa Figueiredo
Rodrigo F. M. de Almeida
Catarina A. C. Antunes
Catarina Garcia
Catarina P. Reis
Lia Ascensão
Rita G. Sobral
Patricia Rijo
Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall Interactions
Biomolecules
7α-Acetoxy-6β-hydroxyroyleanone
MRSA
antibacterial activity
membrane interaction
cell wall
title Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall Interactions
title_full Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall Interactions
title_fullStr Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall Interactions
title_full_unstemmed Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall Interactions
title_short Unveiling the Mechanism of Action of 7α-acetoxy-6β-hydroxyroyleanone on an MRSA/VISA Strain: Membrane and Cell Wall Interactions
title_sort unveiling the mechanism of action of 7α acetoxy 6β hydroxyroyleanone on an mrsa visa strain membrane and cell wall interactions
topic 7α-Acetoxy-6β-hydroxyroyleanone
MRSA
antibacterial activity
membrane interaction
cell wall
url https://www.mdpi.com/2218-273X/10/7/983
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